Absorption of Drugs from the Gastrointestinal Tract

  • L. S. Schanker
Part of the Handbuch der experimentellen Pharmakologie/Handbook of Experimental Pharmacology book series (HEP, volume 28 / 1)

Abstract

Drugs are most often administered to man by the oral route. Compared to other modes of administration, this route is unusually difficult to describe with regard to the physico-chemical conditions existing at the site of absorption. For example, the contents of the gastrointestinal tract vary widely in pH value, volume, viscosity and composition; moreover, the rate of gastric emptying and the degree of intestinal motility are highly variable. Thus a drug is retained in the acidic environment of the stomach for a few minutes or for hours; it is propelled through the duodenal, jejunal and ileal portions of the intestine at varying rates; and it is exposed to innumerable foodstuffs, products of digestion, bacteria and digestive enzymes. As if these variables did not make the oral route difficult enough to characterize, drugs are given orally in a wide array of dosage forms, each with its own set of physical properties: there are tablets, capsules, suspensions, emulsions, a variety of solutions, and specially formulated dosage forms for prolonged or delayed action. It is not surprising then that investigators interested in the mechanisms of gastrointestinal absorption have largely turned to surgically prepared laboratory animals in which one portion of the gastrointestinal tract can be studied at a time, the nature of the luminal contents controlled, and drugs maintained in true aqueous solution.

Keywords

Alkaloid Mannitol Aniline Tetracycline Uracil 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Berggren, S.M., Goldberg, L.: The absorption of ethyl alcohol from the gastrointestinal tract as a diffusion process. Acta physiol. scand. 1, 246–270 (1940).CrossRefGoogle Scholar
  2. Collander, R., Bärlfnd, H.: Permeabilitätsstudien an Chara ceratophylla. II. Die Permeabilität für Nichtelektrolyte. Acta bot. fenn. 11, 1–114 (1933).Google Scholar
  3. Handschumacher, R.E., Creasey, W.A., Fink, M.E., Calabresi, P., Welch, A.D.: Pharmacological and clinical studies with triacetyl 6-azauridine. Cancer Chemother. Rep. 16, 267–269 (1962).PubMedGoogle Scholar
  4. Höber, R.: Physical chemistry of cells and tissues. Philadelphia: Blakiston Co. 1945.Google Scholar
  5. Höber, R., HÖber, J.: Experiments on the absorption of organic solutes in the small intestine of rats. J. cell. comp. Physiol. 10, 401–422 (1937).CrossRefGoogle Scholar
  6. Hoeksema, H., Whitfield, G.B., Rhuland, L.E.: Effect of selective acylation on the oral absorption of a nucleoside by humans. Biochem. biophys. Res. Commun. 6, 213–216 (1961).PubMedCrossRefGoogle Scholar
  7. Hogben, C.A.M., Schanker, L.S., Tocco, D. J., Brodie, B.B.: Absorption of drugs from the stomach. II. The human. J. Pharmacol, exp. Ther. 120, 540–545 (1957).Google Scholar
  8. Hogben, C.A.M., Tocco, D.J., Brodie, B.B., Schanker, L.S.: On the mechanism of intestinal absorption of drugs. J. Pharmacol, exp. Ther. 125, 275–282 (1959).Google Scholar
  9. Kakemi, K., Arita, T., Mujranishi, S.: Absorption and excretion of drugs. XXV. On the mechanism of rectal absorption of sulfonamides. Chem. pharm. Bull. 13, 861–869 (1965).PubMedGoogle Scholar
  10. Lamanna, C.: Toxicity of bacterial exotoxins by the oral route. Science 131, 1100–1101 (1960).PubMedCrossRefGoogle Scholar
  11. Lazarus, J., Cooper, J.: Oral prolonged action medicaments: Their pharmaceutical control and therapeutic aspects. J. Pharm. Pharmacol. 11, 257–290 (1959).PubMedCrossRefGoogle Scholar
  12. Levine, R.R., Pelikan, E.W.: The influence of experimental procedures and dose on the intestinal absorption of an onium compound, benzomethamine. J. Pharmacol, exp. Ther. 131, 319–327 (1961).Google Scholar
  13. Levine, R.R., Pelikan, E.W., Spencer, A.F.: Effect of a phosphatidopeptide fraction of intestinal tissue on the intestinal absorption of a quaternary ammonium compound. Biochem. Pharmacol. 8, 248–250 (1961).PubMedCrossRefGoogle Scholar
  14. Levy, G.: Kinetics and implications of dissolution rate limited gastrointestinal absorption of drugs. In: Physicochemical aspects of drug actions, pp. 33–62. Oxford: Pergamon Press 1968.Google Scholar
  15. Nelson, E.: Kinetics of drug absorption, distribution, metabolism, and excretion. J. pharm. Sci. 50, 181–192 (1961).PubMedCrossRefGoogle Scholar
  16. O’Reilly, I., Nelson, E.: Urinary excretion kinetics for evaluation of drug absorption IV. Studies with tetracycline absorption enhancement factors. J. pharm. Sci. 50, 413–416 (1961).PubMedCrossRefGoogle Scholar
  17. Overton, E.: Beiträge zur allgemeinen Muskel- und Nervenphysiologie. Pflügers Arch. ges. Physiol. 92, 115–280 (1902).CrossRefGoogle Scholar
  18. Pindell, M.H., Cull, K.M., Doran, K.M., Dickison, H.L.: Absorption and excretion studies on tetracycline. J. Pharmacol, exp. Ther. 125, 287–294 (1959).Google Scholar
  19. Schanker, L.S.: Absorption of drugs from the rat colon. J. Pharmacol, exp. Ther. 126, 283–290 (1959).Google Scholar
  20. Schanker, L.S. Passage of drugs across body membranes. Pharmacol. Rev. 14, 501–530 (1962).PubMedGoogle Scholar
  21. Schanker, L.S.: Passage of drugs across the gastrointestinal epithelium. In: Proceedings of the first international pharmacological meeting (C.A.M. HOGBEN, ed.). Vol. 4, pp. 121–130. London: Pergamon Press 1963.Google Scholar
  22. Schanker, L.S. Jeffrey, J. J.: Active transport of foreign pyrimidines across the intestinal epithelium. Nature (Lond.) 190, 727–728 (1961).CrossRefGoogle Scholar
  23. Schanker, L.S.: Structural specificity of the pyrimidine transport process of the small intestine. Biochem. Pharmacol. 11, 961–966 (1962).PubMedCrossRefGoogle Scholar
  24. Schanker, L.S. Johnson, J.M.: Increased intestinal absorption of foreign organic compounds in the presence of ethylenediaminetetraacetic acid (EDTA). Biochem. Pharmacol. 8, 421–422 (1961).PubMedCrossRefGoogle Scholar
  25. Schanker, L.S.: Shore, P.A., Brodie, B.B., Hogben, C.A.M.: Absorption of drugs from the stomach. I. The rat. J. Pharmacol, exp. Ther. 120, 528–539 (1957).Google Scholar
  26. Schanker, L.S., Tocco, D.J.: Active transport of some pyrimidines across the rat intestinal epithelium. J. Pharmacol, exp. Ther. 128, 115–121 (1960).Google Scholar
  27. Schanker, L.S.: Some characteristics of the pyrimidine transport process of the small intestine. Biochim. biophys. Acta (Amst.)56, 469–473 (1962).CrossRefGoogle Scholar
  28. Schanker, L.S., Tocco, D.J., Brodie, B.B., Hogben, C.A.M.: Absorption of drugs from the rat small intestine. J. Pharmacol, exp. Ther. 123, 81–88 (1958).Google Scholar
  29. Schedl, H.P., Clifton, J.A.: Small intestinal absorption of steroids. In: Advance abstracts of short communications, First international congress of endocrinology (F. Fuchs, ed.), p. 741. Copenhagen: Periodica Copenhagen 1960.Google Scholar
  30. Schedl, H.P., Clifton, J.A.: Small intestinal absorption of steroids. Gastroenterology 41, 491–499 (1961).PubMedGoogle Scholar
  31. Shore, P. A., Brodie, B.B., Hogben, C.A.M.: The gastric secretion of drugs: a pH partition hypothesis. J. Pharmacol, exp. Ther. 119, 361–369 (1957).Google Scholar
  32. Travell, J.: The influence of the hydrogen ion concentration on the absorption of alkaloids from the stomach. J. Pharmacol, exp. Ther. 69, 21–33 (1940).Google Scholar
  33. Wagner, J.G.: Biopharmaceutics: absorption aspects. J. pharm. Sci. 50, 359–387 (1961).PubMedCrossRefGoogle Scholar
  34. Wagner, J.G., Nelson, E.: Per cent absorbed time plots derived from blood level and/or urinary excretion data. J. pharm. Sci. 52, 610–611 (1963).PubMedCrossRefGoogle Scholar
  35. Wilson, T.H.: Intestinal absorption. Philadelphia: W.B. Saunders Co. 1962.Google Scholar
  36. Wilson, T.H., Landau, B. R.: Specificity of sugar transport by the intestine of the hamster. Amer. J. Physiol. 198, 99–102 (1960).PubMedGoogle Scholar
  37. Windsor, E., Cronheim, G.E.: Gastro-intestinal absorption of heparin and synthetic heparin- oids. Nature (Lond.) 190, 263–264 (1961).CrossRefGoogle Scholar
  38. Wiseman, G.: Absorption from the intestine. London: Academic Press 1964.Google Scholar

Copyright information

© Springer-Verlag Berlin · Heidelberg 1971

Authors and Affiliations

  • L. S. Schanker

There are no affiliations available

Personalised recommendations